Hydroxyzine from topical phospholipid liposomal formulations: evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model

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Abstract

Hydroxyzine, an effective but sedating Hpantihistamine is given orally to treat allergic skin disorders. This study was performed to assess the peripheral Hrantihistaminic activity and extent of systemic absorption of hydroxyzine from liposomes applied to the skin. Using L-aphosphatidylcholine (PC), small unilamellar vesicles (SUVs) and multilamellar vesicles (MLVs) containing hydroxyzine were prepared. Hydroxyzine in Glaxal Base (GB) was used as the control. Using a randomized, crossover design, each formulation, containing 10 mg of hydroxyzine, was applied to the shaved backs of 6 rabbits (3.08 ±0.05 kg). Histamine-induced wheal tests and blood sampling were performed at designated time intervals up to 24 hours. Compared with baseline, hydroxyzine from all formulations significantly suppressed histamine-induced wheal formation by 75% to 95% for up to 24 hours. Mean maximum suppression, 85% to 94%, occurred from 2 to 6 hours, with no differences among the formulations. The areas of plasma hydroxyzine concentration versus time area under the curve (AUCs) from PC-SUV and PC-MLV, 80.1 ±20.8 and 78.4 ±33.9 ng/mL/h, respectively, were lower than that from GB, 492 ±141 ng/mL/h (P < .05). Only 0.02% to 0.06% of the initial hydroxyzine dose remained on the skin after 24 hours. In this model, hydroxyzine from SUV and MLV had excellent topical H1-antihistaminic activity, and minimal systemic expo-sure occurred. Cetirizine formed in-vivo contributed to some of H1-antihistaminic activity.

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APA

Elzainy, A. A. W., Gu, X., Simons, F. E. R., & Simons, K. J. (2003). Hydroxyzine from topical phospholipid liposomal formulations: evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model. AAPS Journal, 5(4). https://doi.org/10.1016/s0091-6749(03)81172-7

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